Almin Arzu, Bora Doli, Bora Utpal
Department of Chemical Sciences, Tezpur University, Napaam, Tezpur, Assam 784028, India.
Org Biomol Chem. 2025 Jun 18;23(24):5833-5839. doi: 10.1039/d5ob00391a.
A mild and efficient Pd-catalyzed protocol has been developed for the direct synthesis of aryl ketones through a reaction of arylboronic acids (and their ester derivatives) with aromatic as well as aliphatic nitriles. The reaction operates under mild conditions using minimal amounts of PTSA as a cost-effective acid additive and water as the sole solvent, enhancing the sustainability of the process. This method exhibits excellent functional group tolerance and a broad substrate scope, delivering both diaryl and alkyl aryl ketones in moderate to excellent yields. Notably, the utility of this methodology is demonstrated the synthesis of (4-methoxyphenyl)(3,4,5-trimethoxyphenyl)methanone (PHT), a pharmaceutically relevant compound, in a remarkable yield of 96%.
已开发出一种温和且高效的钯催化方法，用于通过芳基硼酸（及其酯衍生物）与芳族和脂肪族腈的反应直接合成芳基酮。该反应在温和条件下进行，使用少量对甲苯磺酸作为经济高效的酸添加剂，水作为唯一溶剂，提高了该过程的可持续性。该方法具有出色的官能团耐受性和广泛的底物范围，能以中等至优异的产率得到二芳基酮和烷基芳基酮。值得注意的是，该方法的实用性在合成药物相关化合物（4-甲氧基苯基）（3,4,5-三甲氧基苯基）甲酮（PHT）中得到了证明，其产率高达96%。
